Cat. No.: HY-148333

MS177

Name: MS177
Brand: MedChemExpress
SKU: HY-148333
Price: 240.00 USD
Availability: InStock
Rating: 5 (3 reviews)

3 Cited Publications

고객리뷰

Based on 3 publication(s) in Google Scholar

MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC₅₀): 12 nM). MS177 effectively depletes both canonical EZH2-PRC2 and noncanonical EZH2-cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
(Pink: EZH2 ligand (HY-W1063360); Blue: Cereblon ligand (HY-41547); Black: linker (HY-140002)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.55%
CAS No.: 2225938-86-1
화학식: C₄₈H₅₅N₁₁O₈
분자량:914.02

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MS177 Chemical Structure

CAS No.: 2225938-86-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC₅₀): 12 nM). MS177 effectively depletes both canonical EZH2-PRC2 and noncanonical EZH2-cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest^[1]. (Pink: EZH2 ligand (HY-W1063360); Blue: Cereblon ligand (HY-41547); Black: linker (HY-140002)).

IC₅₀ & Target

^[1]

EZH2

All PROTACs Isoforms :

All Histone Methyltransferase Isoforms :

In Vitro

MS177 inhibits the enzymatic activities of EZH2-PRC2 (IC₅₀: 7 nM)^[1].
MS177 (5 μM, 24 h) decreases H3K27me3 and increases H3K27activity in HeLa cells^[1].
MS177 (0.1-5 μM, 16 h) effectively degrades cellular EZH2-PRC2 and suppresses global H3K27me3 in EOL-1 cells^[1].
MS177 (0.1-5 μM, 16 h) induces Myc degradation in EOL-1 and MV4 cells^[1].
MS177 (4 days) shows antiproliferation effects in a panel of MLL-r leukaemia cells and samples from patients with AML, with IC₅₀s below 2 μM^[1].
MS177 (0.5-2.5 μM, 24 h) decreases colony-forming capabilities in MV4;11 cells^[1].
MS177 (0.5-2.5 μM, 24 h) slows cell cycle progression and induces MOLM-13 cell apoptosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

AML cell line: MV4;11, MOML-13, RS4;11, KOPN-8 THP-1, EOL-1 (MLL-r cells)
Control cell line: K562 (CML cells)
Patient sample: AML cells
Concentration:

0-100 μM approximately
Incubation Time:

4 days
Result:

Inhibited cell proliferation with IC₅₀s of 0.1-0.57 μM for MLL-r cells, 0.09-1.35 μM for Patient sample, >100 μM for K562 cell.

Western Blot Analysis^[1]

Cell Line:

EOL-1 cell
Concentration:

0.1, 0.5, 1, 2.5, 5 μM
Incubation Time:

16 h
Result:

Depleted EZH2, EED and SUZ12 in a concentration-dependent manner and suppressed global H3K27me3.

In Vivo

MS177 (100 mg/kg, i.p., BID for 6 days) represses tumor growth in PDX animal model of MLL-r AML, and in subcutaneously xenografted MLL-r leukaemia models^[1].
MS177 (50 mg/kg, i.p.) achieves intraplasma concentrations about 1 μM in male Swiss Albino mice^[1].
MS177 (100 mg/kg, i.p., BID for 6 days per week; and 200 mg/ kg, i.p. BID 3 days per week) is well tolerated and lacks apparent toxicity in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

PDX animal model of MLL-r AML^[1]
Dosage:

100 mg/kg
Administration:

Intraperitoneal injection (i.p.), BID for 6 days.
Result:

Inhibited tumor growth and prolonged survival.

Chemical Information

CAS No. 2225938-86-1
Appearance Solid
분자량 914.02
화학식 C₄₈H₅₅N₁₁O₈
Color Light yellow to yellow
SMILES

O=C(C1=CC(C2=CC=C(N3CCN(CCNC(CCOCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)CC3)N=C2)=CC7=C1C=NN7C(C)C)NCC8=C(C)C=C(C)NC8=O
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

All WBIFRT-PCR

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Journal Impact Factor

Cell Mol Gastroenterol Hepatol

RBM39 Enhances Cholangiocarcinoma Growth Through EZH2-mediated WNT7B/β-catenin Pathway. [Abstract]

2025;19(1):101404. PMID: 39278404

MS177 purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025;19(1):101404. [Abstract]

MS177 (10 μM; 48 h) decreased the nuclear localization of β-catenin in HuCCT1 and CCLP1 cells.

MS177 purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025;19(1):101404. [Abstract]

MS177 (10 μM; 48 h) decreased the level of active β-catenin in HuCCT1 and CCLP1 cells.

MS177 purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025;19(1):101404. [Abstract]

MS177 (10 μM; 48 h) revealed a reduction in the nuclear localization of β-catenin in HuCCT1 and CCLP1 cells.

MS177 purchased from MedChemExpress. Usage Cited in: Cell Mol Gastroenterol Hepatol. 2025;19(1):101404. [Abstract]

MS177 (10 μM; 48 h) showed that the mRNA of β-catenin targets (c-Myc, BIRC5, and AXIN2) was markedly downregulated in HuCCT1 and CCLP1 cells.
Biochim Biophys Acta Mol Basis Dis

EZH2 contributes to sepsis-induced acute lung injury through regulating macrophage polarization. [Abstract]

2025 Jan;1871(1):167554. PMID: 39471914
Mol Immunol

Sigmoidin B attenuates sepsis-associated encephalopathy through EZH2-AKT2-mediated regulation of microglial polarization. [Abstract]

2025 Oct:186:95-113. PMID: 40834508

MS177 purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2025 Oct:186:95-113. [Abstract]

MS177 (4 mg/kg) led to a significant reduction in p-AKT2 expression in microglia of SAE mice.

용액&용해도

In Vitro:

DMSO : 100 mg/mL (109.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0941 mL

5.4703 mL

10.9407 mL

5 mM

0.2188 mL

1.0941 mL

2.1881 mL

10 mM

0.1094 mL

0.5470 mL

1.0941 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (2.28 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wang J, et al. EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis. Nat Cell Biol. 2022 Mar;24(3):384-399. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0941 mL	5.4703 mL	10.9407 mL	27.3517 mL
	5 mM	0.2188 mL	1.0941 mL	2.1881 mL	5.4703 mL
	10 mM	0.1094 mL	0.5470 mL	1.0941 mL	2.7352 mL
	15 mM	0.0729 mL	0.3647 mL	0.7294 mL	1.8234 mL
	20 mM	0.0547 mL	0.2735 mL	0.5470 mL	1.3676 mL
	25 mM	0.0438 mL	0.2188 mL	0.4376 mL	1.0941 mL
	30 mM	0.0365 mL	0.1823 mL	0.3647 mL	0.9117 mL
	40 mM	0.0274 mL	0.1368 mL	0.2735 mL	0.6838 mL
	50 mM	0.0219 mL	0.1094 mL	0.2188 mL	0.5470 mL
	60 mM	0.0182 mL	0.0912 mL	0.1823 mL	0.4559 mL
	80 mM	0.0137 mL	0.0684 mL	0.1368 mL	0.3419 mL
	100 mM	0.0109 mL	0.0547 mL	0.1094 mL	0.2735 mL

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MS177

Publications Citing Use of MedChemExpress (MCE) MS177

All PROTACs Isoforms

All Histone Methyltransferase Isoforms